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以赖氨酸盐形式给药的阿司匹林的药代动力学中的给药途径和性别差异。

Route of administration and sex differences in the pharmacokinetics of aspirin, administered as its lysine salt.

作者信息

Aarons L, Hopkins K, Rowland M, Brossel S, Thiercelin J F

机构信息

Department of Pharmacy, University of Manchester, U.K.

出版信息

Pharm Res. 1989 Aug;6(8):660-6. doi: 10.1023/a:1015978104017.

Abstract

One thousand milligrams of aspirin, as its lysine salt was administered intravenously, orally, and intramuscularly to nine male and nine female young healthy adult volunteers. After intravenous injection mean (+/- SD) values of clearance, steady-state volume of distribution, and terminal half-life were 12.2 +/- 2.2 ml/min/kg, 0.219 +/- 0.042 liter/kg, and 15.4 +/- 2.5 min, respectively, with no differences between males and females. Following administration aspirin was absorbed more quickly in females than in males (mean absorption times of 16.4 and 21.3 min, respectively although the bioavailability, 54%, was the same in both groups. In contrast, following intramuscular administration, aspirin was absorbed more slowly in females than males (mean absorption time of 97 and 53 min, respectively) but again the bioavailability, 89%, was the same in both groups. The data suggest that in the female the intramuscular injection is going into fat. Salicylic acid concentration-time profiles showed a less pronounced sex difference and were comparable among the routes of administration.

摘要

将1000毫克阿司匹林赖氨酸盐分别通过静脉、口服和肌肉注射的方式给予9名年轻健康成年男性志愿者和9名年轻健康成年女性志愿者。静脉注射后,清除率、稳态分布容积和末端半衰期的平均(±标准差)值分别为12.2±2.2毫升/分钟/千克、0.219±0.042升/千克和15.4±2.5分钟,男性和女性之间无差异。给药后,阿司匹林在女性体内的吸收速度比男性快(平均吸收时间分别为16.4分钟和21.3分钟),尽管两组的生物利用度均为54%。相比之下,肌肉注射后,阿司匹林在女性体内的吸收速度比男性慢(平均吸收时间分别为97分钟和53分钟),但两组的生物利用度同样均为89%。数据表明,在女性中,肌肉注射的药物进入了脂肪组织。水杨酸浓度-时间曲线显示出较小的性别差异,且在不同给药途径之间具有可比性。

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